The present invention relates to cephalosporin derivatives with improved pharmacokinetics, to a process for their preparation and to pharmaceutical compositions in which they are present. It further relates to a novel intermediate for synthesizing certain of the cephalosporin derivatives.
In French patent application no. 84 14 878 published on Mar. 28, 1986 under the number 2 570 702, the Applicant Company described a family of cephalosporin derivatives possessing a broad activity against both Gram-negative germs and Gram-positive germs.
These derivatives include, in particular, compounds substituted in the 3-position by a group: ##STR4## in which Alk represents an optionally substituted lower alkylene group and in which the substituent --NH--CO--Alk--NH.sub.2 is located in the 3-position or 4-position.
According to the present invention, it has been found, surprisingly, that by slightly modifying the nature of the substituent in the 3-position, compounds are obtained which preserve the good activity of the compounds described in the prior art but additionally have greatly improved pharmacokinetic properties and, in particular, very high plasma concentrations which persist over a very long period.
Modification of the pharmacokinetic parameters in this way is important inasmuch as it opens up the possibility of reducing the dosage and the number of administrations of the product required for the same therapeutic effect.